Daunorubicin and doxorubicin, anthracycline antibiotics, a physicochemical and biological review.

Article Details

Citation

Aubel-Sadron G, Londos-Gagliardi D

Daunorubicin and doxorubicin, anthracycline antibiotics, a physicochemical and biological review.

Biochimie. 1984 May;66(5):333-52.

PubMed ID
6380596 [ View in PubMed
]
Abstract

Daunorubicin and doxorubicin, two antibiotics belonging to the anthracycline group, are widely used in human cancer chemotherapy. Their activity has been attributed mainly to their intercalation between the base pairs of native DNA. Complex formation between daunorubicin or doxorubicin with polydeoxyribonucleotides and DNAs of various base composition or chromatins has been investigated by numerous techniques. Many authors have tried to correlate biological and therapeutic activities with the affinity of the drugs for DNA or some specific sequences of DNA. In vivo these anthracycline drugs cause DNA damage such as fragmentation and single-strand breaks. The mechanism of action of anthracyclines involves the inhibition of RNA and DNA syntheses. There exists two limiting factors in the use of anthracyclines as antitumoral agents: a chronic or acute cardiotoxicity and a spontaneous or acquired resistance. In both cases, there is probably an action at the membrane level. It has to be noted that daunorubicin and doxorubicin have a particular affinity for phospholipids and that the development of resistance is linked to some membrane alterations.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
DaunorubicinDNANucleotideHumans
Yes
Intercalation
Details
DaunorubicinDNA topoisomerase 2-alphaProteinHumans
Yes
Inhibitor
Details
DaunorubicinDNA topoisomerase 2-betaProteinHumans
Yes
Inhibitor
Details